The NIH opiate total synthesis (previously reported) now renders the total synthesis of either enantiomer of codeine, morphine and thebaine possible in about 25% overall yield from m-methoxyphenethylamine with only 6-8 isolated intermediates. These results can now provide, for the first time, a commercial source of medical opiates which is independent of the opium poppy. The route has now been extended to provide a practical, thebaine-free total synthesis of N-cycloalkylmethylnorthebaine derivatives which are valuable intermediates for total synthesis of narcotic antagonist and agonist-antagonist drugs. Using commercially available m-methoxyphenethylamine as starting material either optical isomer of N-cyclopropylmethyl- and N-cyclobutylmethylnorthebaine can be synthesized in about 20% overall yield. The natural enantiomers of naltrexone and nalbuphine have now been prepared from these intermediates, respectively. In addition, the unnatural enantiomers of oxymorphone, codeine, morphine, naloxone, and naltrexone have been prepared by the NIH total synthesis. The latter two compounds have proven to be valuable research tools in several lines of opiate research including characterization of the newly discovered lambda opiate binding site. Since this site only binds 4,5-epoxymorphinans, the unnatural opiate enantiomers were an absolute requirement. Further studies with these compounds are in progress.